肺靶向甲强龙琥珀酸钠明胶微球的制备

Preperation of Lung Targeting Gelatin Microspheres of Methylprednisolone Sodium Succinate

目的:探讨肺靶向甲强龙琥珀酸钠明胶微球的制备、稳定性及体外释药特性。方法:采用二步法制备肺靶向甲强龙琥珀酸钠明胶微球,并结合甲强龙琥珀酸钠的水解特性测定其载药量和体外释药特性。结果:制备出吸胀后平均算术粒径(9.9±3.5)μm的微球,515μm的微球占82.7%,载药量20.5%,在pH7.4PBS缓冲液中的释药规律符合Weibull方程,t1/2为43.5min。微球在室温下放置3个月形态及载药量无明显改变。结论:本方法制备的甲强龙琥珀酸钠明胶微球可用于肺靶向治疗。

Objective： To study the preparation techniques, stability and the release profile in vitro of gelatin microspheres （GMS） encapsulated with methylprednisolone sodium succinate （MPS）. Methods. Gelatin microspheres of methylprednisolone sodium succinate （MPS-GMS）were prepared by the two-step method, their drug contents which were corrected by the hydrolytic profile of MPS, and their release profile in vitro was studied. Results： The arithmetic mean diameter of MPS-GMS was 9.9±3.5 μm after swelling. There were 82.7% of the microspheres ranging from 5 to 15 μm. The drug content was 20.5%. The release profile in vitro （pH7.4 phoshate buffer） can be described by the Weibull equation. The t1/2 value was 43.5 min. The shape and drug content were stable for three months when stored at room temperature. Conclusion： MPS-GMS can be used for treatment of lung target.